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Copyright @ Pol J Cosmetol
Pol J Cosmetol 2020, 23(3): 159-165pl  Products of the catalytic oxyethylation of ketoprofen as new potential prodrugsMarian M. Zgoda 1/, Michał K. Kołodziejczyk 2/, Michał Nachajski 2/, Marek Lukosek 3/, Jacek Kosno 3/, Sławomira Nowak 4/ 1/ Wyższa Szkoła Kosmetyki i Nauk o Zdrowiu w Łodzi 2/ Zakład Technologii Postaci Leków Katedra Farmacji Stosowanej Uniwersytetu Medycznego w Łodzi 3/ Zakład Środków Powierzchniowo Czynnych ICSO "Blachownia" Kędzierzyn Koźle 4/ Katedra i Zakład Farmakognozji Uniwersytetu Medycznego w Łodzi Summary Introduction. Innovative research was carried out on the polarity of the ketoprofen through the catalytic process of oxyethylation by ethylene oxide. The obtained prodrugs will be the basis for pre-formulation research on the forms of preparations applied to the skin and cosmetic preparations with analgesic and anti-inflammatory effect. Aim. The aim of the research was to develop the synthesis of oxyethylated derivative of ketoprofen with significantly increased water solubility and hydrodynamic parameters of the molecule, which will have an analgesic effect without the transdermal passage promoter. Material and methods. The catalytic process of ketoprofen oxyethylation was carried out in ICSO "Blachownia" in Kędzierzyn Koźle. The obtained products were subjected to GPC chromatographic analysis before and after purification on activated carbon. The molecular weights of the derivatives (Mw, Mp, Mη), the content of oxyethylene segments (E%) and the level of hydrophilic-lipophilic balance were determined. Measurement of the viscosities of methanol and aqueous solutions of derivatives made it possible to calculate the hydrodynamic parameters of the prodrug molecules. Results. The oxyethylation of ketoprofen and purification make it possible to obtain a product with a low content of polyethylene glycols. The HLB level of the prodrug with nTE=20 and nTE=60 and the calculated radius of the derivative molecule indicate that they will diffuse into a tissue compartment without the transdermal passage promoter. Conclusions. The developed technology enables pre-formulation work to produce the original form of a preparation applied to the skin and effective anti-inflammatory and analgesic cosmetic. Key words: ketoprofen, oxyethylated derivative, GPC chromatography, viscosity, hydrodynamic parameters |